Pharmaceutical compositions for oral administration are typically required to exhibit not only stability of the active ingredient, but also excellent absorbability during oral administration; and mass production methods of the compositions are also required.
In crystals, there may be polymorphs that contain the same molecule but have different molecular arrangements. Such polymorphs are known to exhibit different peaks in X-ray powder diffraction measurement (XRD measurement). Additionally, those crystal polymorphs are known to exhibit different solubility, oral absorbability, stability, and the like. Thus, optimal crystals must be found from different perspectives in developing drugs.
At present, a number of FGFR inhibitors are reported as antitumor agents, and Patent Literature 1, 2, and 3 disclose (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-1-pyrrolidinyl)-2-propen-1-one (hereinafter “compound 1”) as a compound that has excellent FGFR inhibitory activity and that exhibits antitumor activity.

However, none of Patent Literature 1, 2, or 3 discloses or suggests the crystal of compound 1, and the stability, oral absorbability, and crystallization method of the crystal.